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More than 5000 active chemicals with high quality for research!
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(R)-STU104 is a potent, first-in-class TAK1-MKK3 porotein-protein interaction (PPI) inhibitor with SPR Kd of 71 nM for binding MKK3, disrupting the TAK1 phosphorylating MKK3.(R)-STU104 exhibited the potent inhibitory activity on TNF-α production on RAW264.7 cells with IC50 of 0.58 uM, suppressed the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways.(R)-STU104 demonstrated remarkable dose-effect relationships on both acute and chronic mouse ulcerative colitis (UC) models.(R)-STU104 showed better anti-UC efficacy in vivo at 10 mg/kg/d than mesalazine at the dose of 50 mg/kg/d.
HRX-0233 (HRX0233) is a potent and selective inhibitor of MAP2K4 (MKK4), a kinase involved in the stress-activated protein kinase (SAPK) signaling pathway. MAP2K4 plays a role in regulating cellular responses to stress, apoptosis, and tumorigenesis. HRX-0233 has shown particular promise in KRAS-mutant cancers, where it exhibits synergistic effects with RAS inhibitors, making it a potential candidate for combination therapy in these difficult-to-treat cancers.
Darizmetinib (HRX-0215, HRX0215) is a potent, selective inhibitor of MKK4 (MAP2K4/SEK1), shows potential for promoting liver regeneration or reducing or preventing hepatocyte death.
INR119 is a small molecule allosteric MAPKK (MAP2K, MEK1/2) inhibitor, binds fission yeast homologue Wis1 near C458 and protects Wis1 from inactivation by low levels of H2O2 in vitro.INR119 pretreatment strongly potentiates the Wis1 response to low H2O2 in vivo.Phosphorylation of Sty1 depends entirely on activated Wis1, and the INR119-induced enhancement of Sty1 pathway activation upon H2O2 stress requires the upstream activation of Wis1 through the MAPKKKs.
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site.
KZ-001 is a highly potent and selective MEK 1/2 inhibitor with IC50 values of 7.4/64 nM, respectively, exhibits greater inhibition against BRAF- and KRAS-mutant tumor cells than AZD6244.
DS03090629 is a potent, selective, ATP-competitive and orally available MEK1/2 inhibitor, shows high affinity for the MEK protein regardless of its phosphorylation status (npMEK (inactive) Kd=0.11 nM, and pMEK (active) Kd=0.15 nM).
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